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Experimental Methods to Determine Binding Kinetics
Book Contribution - Chapter
Drugs interact with proteins and that interaction leads to the pharmacological
response. The interaction involves an initial binding of the drug to the protein,
described by the second order association rate constant, k on and debinding,
described by the ?rst-order dissociation rate constant, k o? . The a?nity of the
drug for the protein is de?ned by the equilibrium dissociation constant, K d ,
which equals k o? /k on . It is recognized that biology is not at equilibrium and for
some situations binding kinetics (k on and k o? ) may be a better predictor of a
pharmacological response than the equilibrium constant.
response. The interaction involves an initial binding of the drug to the protein,
described by the second order association rate constant, k on and debinding,
described by the ?rst-order dissociation rate constant, k o? . The a?nity of the
drug for the protein is de?ned by the equilibrium dissociation constant, K d ,
which equals k o? /k on . It is recognized that biology is not at equilibrium and for
some situations binding kinetics (k on and k o? ) may be a better predictor of a
pharmacological response than the equilibrium constant.
Book: Kinetics and Thermodynamics of Drug binding
Series: Wiley's Methods and Principles in Medicinal Chemistry Series
Pages: 169-189
Number of pages: 21
ISBN:978-3-527-33582-4
Publication year:2015
Keywords:binding kinetics, radioligand, surface plasmon resonance, enzyme activity